| Name | H-151 |
| Description | H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammatory diseases in vivo and ex vivo. |
| In vitro | METHODS: Mouse monocyte macrophage RAW264.7 was treated with H-151 (0.25-2 μM) for 1 h, and then stimulated with rmCIRP (1 μg/mL) for 24 h. The level of IFN-β was measured by ELISA.
RESULTS: IFN-β was dose-dependently reduced in the culture supernatant of cells pretreated with H-151, which inhibited eCIRP-induced activation of STING in vitro. [1]
METHODS: Human monocytes THP-1 were treated with H-151 (0.5 μM) for 2 h, and the expression levels of target proteins were measured by Western Blot.
RESULTS: H-151 inhibited the phosphorylation of TBK1, and H-151 effectively inhibited the activation of hsSTING. [2] |
| In vivo | METHODS: To assay in vivo activity, H-151 (750 nmol, 200 μL) was administered intraperitoneally to Trex1-/- Ifnb1Δβ-luc/Δβ-luc reporter mice once daily for seven days.
RESULTS: When administered for one week, H-151 showed significant efficacy in Trex1-/- mice expressing a bioluminescent IFNβ reporter gene. [2]
METHODS: To test the role in cisplatin-induced acute kidney injury (AKI), H-151 (7 mg/kg) was administered intraperitoneally to C57BL/6J mice with cisplatin-induced AKI three times a day.
RESULTS: H-151 treatment significantly ameliorated cisplatin-induced renal injury, as evidenced by improvement in renal function, renal morphology, and renal inflammation.H-151 may be a potential therapeutic agent for the treatment of AKI, possibly by inhibiting STING-mediated inflammation and mitochondrial damage. [3] |
| Storage | Keep away from moisture | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 12.5 mg/mL (44.75 mM), Suspension.
Ethanol : 14.08 mg/mL (50.4 mM), Sonication is recommended.
DMSO : 100 mg/mL (357.99 mM), Sonication is recommended.
5% DMSO+40% PEG300+5% Tween 80+50% Saline : 5 mg/mL (17.9 mM)
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| Keywords | TMEM173 | TBK1 | STING | Stimulator of Interferon Genes | phosphorylation | palmitoylatio | MPYS | MITA | Inhibitor | inhibit | H-151 | H151 | H 151 | ERIS | autoinflammatory |
| Inhibitors Related | 2',3'-cGAMP sodium | SR-717 | ChX710 | STING ligand-1 | STING agonist-4 | SN-008 | diABZI STING agonist-1 | C-176 | Cridanimod | CCCP | diABZI STING agonist-1 trihydrochloride | C-178 |
| Related Compound Libraries | Nonsteroidal Anti-Inflammatory Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | NO PAINS Compound Library | Immuno-Oncology Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library |
United States
